<abstract xmlns="http://www.w3.org/1999/xhtml">

<sec><h3>Objective</h3>
<p>The objective of the present investigation is to improve the solubility of valsartan and prepare immediate release tablets.</p>
</sec>
<sec><h3>Materials and methods</h3>
<p>To increase the solubility and bioavailability of valsartan, a low-soluble antihypertensive drug, immediate release dosage forms were formulated by a direct compression method using a solid dispersion technique with three different carriers (β-cyclodextrin, polyvinyl pyrrolidone K30 and poloxamer 188) at three different ratios (1:3, 1:4 and 1:5). Nine physical mixtures (PM1–PM9) were prepared and various physical parameters were characterised in <italic>in vitro</italic> release studies.</p>
</sec>
<sec><h3>Results</h3>
<p>Out of the prepared physical mixtures, PM8 showed the best results, with 94.2% of the drug dissolving within 30 min. Formulation PM8 solid dispersion further used for the preparation of valsartan immediate release tablets by using sodium starch glycolate superdisintegrant, at different concentrations (3%, 4% and 5%; i.e., IF1, IF2 and IF3 formulations, respectively). The optimised formulation showed friability and disintegration values of 0.456±0.9 and 6.2±0.4 min. Among the three immediate release formulations, IF2, which contains 4% sodium starch glycolate, demonstrated an 84.46% drug release in 30 min and a 99.69% drug release in 1 hr, indicating increased drug solubility. When compared with a valsartan pure drug, the solubility of the solid dispersion increased by 135.06-fold.</p>
</sec>
<sec><h3>Discussion and conclusion</h3>
<p>The results show that the optimised IF2 formulation demonstrated enhanced drug solubility by 135.06-fold, using a solid dispersion technique with poloxamer 188. This can be explained by the conversion of crystalline to an amorphous form of drug, leading to a reduction in the contact angle between the drug and the gastric medium. It can be concluded that poloxamer 188 is a suitable carrier and that use of a physical mixture technique is an applicable method to improve the solubility of valsartan.</p>
</sec>
</abstract>

Objective
The objective of the present investigation is to improve the solubility of valsartan and prepare immediate release tablets.

Materials and methods
To increase the solubility and bioavailability of valsartan, a low-soluble antihypertensive drug, immediate release dosage forms were formulated by a direct compression method using a solid dispersion technique with three different carriers (β-cyclodextrin, polyvinyl pyrrolidone K30 and poloxamer 188) at three different ratios (1:3, 1:4 and 1:5). Nine physical mixtures (PM1–PM9) were prepared and various physical parameters were characterised in in vitro release studies.

Results
Out of the prepared physical mixtures, PM8 showed the best results, with 94.2% of the drug dissolving within 30 min. Formulation PM8 solid dispersion further used for the preparation of valsartan immediate release tablets by using sodium starch glycolate superdisintegrant, at different concentrations (3%, 4% and 5%; i.e., IF1, IF2 and IF3 formulations, respectively). The optimised formulation showed friability and disintegration values of 0.456±0.9 and 6.2±0.4 min. Among the three immediate release formulations, IF2, which contains 4% sodium starch glycolate, demonstrated an 84.46% drug release in 30 min and a 99.69% drug release in 1 hr, indicating increased drug solubility. When compared with a valsartan pure drug, the solubility of the solid dispersion increased by 135.06-fold.

Discussion and conclusion
The results show that the optimised IF2 formulation demonstrated enhanced drug solubility by 135.06-fold, using a solid dispersion technique with poloxamer 188. This can be explained by the conversion of crystalline to an amorphous form of drug, leading to a reduction in the contact angle between the drug and the gastric medium. It can be concluded that poloxamer 188 is a suitable carrier and that use of a physical mixture technique is an applicable method to improve the solubility of valsartan.

Development and Characterisation of Valsartan Immediate Release Dosage Form Using Solubility Enhancement Technique

Centurion University of Technology and Management

European Pharmaceutical Journal

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 International License.

Objective
The objective of the present investigation is to improve the solubility of valsartan and prepare immediate release tablets.

Materials and methods
To...

Development and Characterisation of Valsartan Immediate Release Dosage Form Using Solubility Enhancement Technique

Article Category: Original Paper

Published Online: Jun 07, 2024

Page range: -

Received: Dec 29, 2023

Accepted: Apr 04, 2024

DOI: https://doi.org/10.2478/afpuc-2024-0005

Keywords
Immediate release tablets, valsartan, β-cyclodextrin, poly vinyl pyrrolidone K30, Poloxamer 188, Physical mixture

© 2024 R. Saripilli et al., published by Sciendo

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 International License.

Development and Characterisation of Valsartan Immediate Release Dosage Form Using Solubility Enhancement Technique

Article Category: Original Paper

Published Online: Jun 07, 2024

Page range: -

Received: Dec 29, 2023

Accepted: Apr 04, 2024

DOI: https://doi.org/10.2478/afpuc-2024-0005

KeywordsImmediate release tablets, valsartan, β-cyclodextrin, poly vinyl pyrrolidone K30, Poloxamer 188, Physical mixture

© 2024 R. Saripilli et al., published by Sciendo

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 International License.

Keywords
Immediate release tablets, valsartan, β-cyclodextrin, poly vinyl pyrrolidone K30, Poloxamer 188, Physical mixture